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Assay Detail

CHEMBL754205

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity by inhibition of [3H]DAMGO binding to Opioid receptor mu 1 from rat brain membranes
45
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.
Boyd RE, Carson JR, Codd EE, Gauthier AD, Neilson LA, Zhang SP.
Bioorg Med Chem Lett (2000) 10 : 1109 -1111
PubMed 10843229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 6.16 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 8.74
CHEMBL13169 1 7.89
CHEMBL12752 1 7.64
CHEMBL275011 1 7.03
CHEMBL13414 1 6.95
CHEMBL275135 1 6.91
CHEMBL13309 1 6.89
CHEMBL275288 1 6.89
CHEMBL13479 1 6.76
CHEMBL274167 1 6.61
CHEMBL273929 1 6.60
CHEMBL13327 2 6.53
CHEMBL273404 1 6.51
CHEMBL13371 1 6.46
CHEMBL268941 1 6.43
CHEMBL13301 1 6.43
CHEMBL264948 1 6.15
CHEMBL13691 1 6.09
CHEMBL13725 1 6.09
CHEMBL13493 1 6.07
CHEMBL13292 1 6.01
CHEMBL13403 1 5.94
CHEMBL13055 1 5.93
CHEMBL276243 1 5.92
CHEMBL13470 SNC-80 1 5.89
CHEMBL13360 1 5.87
CHEMBL406783 1 5.85
CHEMBL12828 1 5.85
CHEMBL13393 1 5.80
CHEMBL13454 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE Ki = 1.8 nM 8.74
CHEMBL13169 Ki = 13.0 nM 7.89
CHEMBL12752 Ki = 23.0 nM 7.64
CHEMBL275011 Ki = 94.0 nM 7.03
CHEMBL13414 Ki = 113.0 nM 6.95
CHEMBL275135 Ki = 124.0 nM 6.91
CHEMBL275288 Ki = 130.0 nM 6.89
CHEMBL13309 Ki = 128.0 nM 6.89
CHEMBL13479 Ki = 172.0 nM 6.76
CHEMBL274167 Ki = 244.0 nM 6.61
CHEMBL273929 Ki = 249.0 nM 6.60
CHEMBL13327 Ki = 293.0 nM 6.53
CHEMBL13327 Ki = 308.0 nM 6.51
CHEMBL273404 Ki = 311.0 nM 6.51
CHEMBL13371 Ki = 350.0 nM 6.46
CHEMBL268941 Ki = 370.0 nM 6.43
CHEMBL13301 Ki = 371.0 nM 6.43
CHEMBL264948 Ki = 704.0 nM 6.15
CHEMBL13725 Ki = 817.0 nM 6.09
CHEMBL13691 Ki = 818.0 nM 6.09
CHEMBL13493 Ki = 845.0 nM 6.07
CHEMBL13292 Ki = 975.0 nM 6.01
CHEMBL13403 Ki = 1155.0 nM 5.94
CHEMBL13055 Ki = 1185.0 nM 5.93
CHEMBL276243 Ki = 1205.0 nM 5.92
CHEMBL13470 SNC-80 Ki = 1300.0 nM 5.89
CHEMBL13360 Ki = 1343.0 nM 5.87
CHEMBL12828 Ki = 1400.0 nM 5.85
CHEMBL406783 Ki = 1420.0 nM 5.85
CHEMBL13393 Ki = 1590.0 nM 5.80
CHEMBL13454 Ki = 1725.0 nM 5.76
CHEMBL269697 Ki = 1820.0 nM 5.74
CHEMBL12765 Ki = 1850.0 nM 5.73
CHEMBL13616 Ki = 2525.0 nM 5.60
CHEMBL274650 Ki = 2773.0 nM 5.56
CHEMBL268981 Ki = 2770.0 nM 5.56
CHEMBL13420 Ki = 2950.0 nM 5.53
CHEMBL13374 Ki = 3018.0 nM 5.52
CHEMBL12912 Ki = 3700.0 nM 5.43
CHEMBL13316 Ki = 4346.0 nM 5.36
CHEMBL13143 Ki = 4830.0 nM 5.32
CHEMBL274125 Ki = 5040.0 nM 5.30
CHEMBL13286 Ki = 5790.0 nM 5.24
CHEMBL13146 Ki = 6350.0 nM 5.20
CHEMBL441905 Ki = 7500.0 nM 5.12